Structure–activity relationships of epolactaene analogs as DNA polymerases inhibitors Original Research Article

Epolactaene, a neuritogenic compound in human neuroblastoma cells, showed inhibitory activities against DNA polymerases α and β. The synthesis and inhibitory activities of epolactaene analogs are described. The α,β-epoxy-γ-lactam moiety in the core and the length of the side chain greatly influenced the activities. Compound 5 was the strongest inhibitor of DNA polymerase α and β of all synthesized compounds with IC50 values of 13 and 78 μM, respectively. N- and O-alkyl derivatives that had modified core moieties showed moderate inhibition.